Figure. Concentration-dependent activation of APLNR by apelin‐13

Reporter cells were transfected with either the expression plasmid for human apelin receptor (APLNR) or the mock plasmid and treated with various concentrations of apelin‐13. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 8.1 nM.

apelin receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Cardiology, Human non-orphan GPCRs

Apelin receptor

The apelin receptor responds to apelin, a 36 amino-acid peptide derived initially from bovine stomach. apelin-36, apelin-13 and [Pyr1]apelin-13 are the predominant endogenous ligands which are cleaved from a 77 amino-acid precursor peptide (APLN, Q9ULZ1) by a so far unidentified enzymatic pathway [1]. A second family of peptides discovered independently and named Elabela [2] or Toddler, that has little sequence similarity to apelin, is present, and functional at the apelin receptor in the adult cardiovascular system [3,4]. Structure-activity relationship Elabela analogues have been described [5].


  1. Tatemoto K, Hosoya M, Habata Y, et al. Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor. Biochem Biophys Res Commun 1998;251:471-6.
  2. Chng SC, Ho L, Tian J, et al. ELABELA: a hormone essential for heart development signals via the apelin receptor. Dev Cell 2013;27:672-80.
  3. Yang P, Read C, Kuc RE, et al. Elabela/Toddler Is an Endogenous Agonist of the Apelin APJ Receptor in the Adult Cardiovascular System, and Exogenous Administration of the Peptide Compensates for the Downregulation of Its Expression in Pulmonary Arterial Hypertension. Circulation 2017;135:1160-1173.
  4. Pauli A, Norris ML, Valen E, et al. Toddler: an embryonic signal that promotes cell movement via Apelin receptors. Science 2014;343:1248636.
  5. Murza A, Sainsily X, Coquerel D, et al. Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions. J Med Chem 2016;59:2962-72.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

Filters Sort results
Reset Apply